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Rpn11-IN-1 Sale

(Synonyms: Capzimin intermediate) 目录号 : GC32407

Rpn11-IN-1是一种有效的选择性蛋白酶体亚基Rpn11抑制剂,IC50为390nM。

Rpn11-IN-1 Chemical Structure

Cas No.:2084867-65-0

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

293T, A549 and HCT 116 cell lines are cultured in DMEM with 10% FBS in white, clear-bottom tissue culture-treated 96-well plates. Cells are treated with different concentrations of inhibitor compounds (e.g., Rpn11-IN-1; 0.01, 0.1, 1, 10, and 100 μM) in triplicates for 72 h at 37°C with 5% CO2 in air. CellTiter-Glo reagent is added to the 96 well plates to measure cell viability. Luminescence values are measured in PHERAstar microplate reader. Collected data is normalized to DMSO control and fit to a dose-response equation to determine IC50 values[1].

References:

[1]. Perez C, et al. Discovery of an Inhibitor of the Proteasome Subunit Rpn11. J Med Chem. 2017 Feb 23;60(4):1343-1361.

产品描述

Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.

Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. When inhibition of Rpn11-IN-1 (Compound 35) against Rpn11 is measured in the presence of Zn(cyclen)2+ (100 μM), a significant loss in activity against Rpn11 is observed (IC50=77.4 μM vs. 0.39 μM). The observed IC50 value shift is attributed to the ability of Zn(cyclen)2+ to compete/titrate Rpn11-IN-1 away from Rpn11. Rpn11-IN-1 blocks proliferation of tumor cells in culture. Rpn11-IN-1 has an IC50 of 2.1 μM and 3.8 μM against 293T and A549 cells, respectively[1].

[1]. Perez C, et al. Discovery of an Inhibitor of the Proteasome Subunit Rpn11. J Med Chem. 2017 Feb 23;60(4):1343-1361.

Chemical Properties

Cas No. 2084867-65-0 SDF
别名 Capzimin intermediate
Canonical SMILES SC1=CC=CC2=C1N=CC(C(NCCC3=NC=CS3)=O)=C2
分子式 C15H13N3OS2 分子量 315.41
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 3.1705 mL 15.8524 mL 31.7048 mL
5 mM 0.6341 mL 3.1705 mL 6.341 mL
10 mM 0.317 mL 1.5852 mL 3.1705 mL
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